C07J31/00

METHODS FOR THE PREPARATION OF OBETICHOLIC ACID AND DERIVATIVES THEREOF
20190062367 · 2019-02-28 ·

The present application relates to a method of preparing a bile acid derivative, or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising direct alkylation at the C-6 position of KLCA.

Process for preparing bile acid derivatives

The present invention relates to processes for preparing compounds of formula I or a pharmaceutically acceptable salt or solvate thereof, wherein the dashed bond (----) at position 7 indicates that the substituent is in an or stereochemistry; R is hydrogen or hydroxy; and R.sub.1 is hydrogen or C.sub.1-C.sub.6 alkyl ##STR00001##

Pharmaceutical compositions and methods of use of 4-pregenen-11?-17-21-triol-3,20-dione derivatives
10188667 · 2019-01-29 · ·

The present invention relates to pharmaceutical compositions comprising 4-pregenen-11?-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

Substituted aryl onium materials

Acid generators comprising a carbocyclic or heteroaromatic group substituted with at least one diester moiety are provided. These acid generators are particularly useful as a photoresist composition component.

Crystalline forms of S-[4-(3-fluoro-3-methylbutyryloxy)but-2-ynyl] 6-α,9-α-difluoro-17-α-(furan-2-yl)carbonyloxy-11-β-hydroxy-16-α-methyl-3-oxoandrosta-1,4-diene-17-β-carbothioate

The present invention relates to crystalline forms of S-[4-(3-fluoro-3-methylbutyryloxy)but-2-ynyl] 6,9-difluoro-17-(furan-2-yl)carbonyloxy-11-hydroxy-16-methyl-3-oxoandrosta-1,4-diene-17-carbothioate, an anti-inflammatory and anti-allergic glucocorticoid compound.

Sulfonium salt, resist composition, and patterning process

On use of a sulfonium salt of specific structure as PAG, acid diffusion is suppressed. A resist composition comprising the sulfonium salt forms a pattern with improved lithography properties including EL, MEF and LWR when processed by lithography.

Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

PHARMACEUTICAL COMPOSITION FOR PREVENTION, TREATMENT OR DELAY OF ALZHEIMER'S DISEASE OR DEMENTIA CONTAINING G PROTEIN-COUPLED RECEPTOR 19 AGENT AS ACTIVE INGREDIENT
20190000863 · 2019-01-03 ·

The present invention relates to a pharmaceutical composition for preventing, treating or delaying an Alzheimer's disease (AD) or dementia including a G protein-coupled receptor19 (GPCR19) agonist or its pharmaceutically acceptable salt as an active ingredient and a food composition for preventing, treating or delaying an Alzheimer's disease or dementia. The GPCR19 agonist according to the present invention has an effect of improving cognitive and behavioral disorders without harming the health of objects when administrated to the objects and has an effect of preventing the Alzheimer's disease or dementia or delaying or treating the progression of the disease in the objects with the disease by suppressing apoptosis of the brain tissue, enhancing immunity, and reducing formation of an amyloid (A) plague.

SELECTIVE PROGESTERONE RECEPTOR MODULATORS (SPRM) AND STABILIZED ESTROGEN LEVEL IN PATIENT

The present invention is related to Selective Progesterone Receptor Modulators (SPRM) as described and defined herein, and covers the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of sexual hormone dependent diseases and gynaecological diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estradiol concentration of treated women is maintained to a level in a range of 40 pg/mL to 85 pg/mL.

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Compounds are provided according to Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):

##STR00002##

and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.